JP7313354B2 - Ｔｌｒ阻害剤として有用なアミド置換されたインドール化合物 - Google Patents

Ｔｌｒ阻害剤として有用なアミド置換されたインドール化合物 Download PDF

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JP7313354B2
JP7313354B2 JP2020534509A JP2020534509A JP7313354B2 JP 7313354 B2 JP7313354 B2 JP 7313354B2 JP 2020534509 A JP2020534509 A JP 2020534509A JP 2020534509 A JP2020534509 A JP 2020534509A JP 7313354 B2 JP7313354 B2 JP 7313354B2
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isopropyl
indol
methylpyridin
indole
ethyl
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JP2021506923A5 (fr
JP2021506923A (ja
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アラリック・ジェイ・ディックマン
ダームパル・エス・ドッド
クリストファー・ピー・マッサリ
トレバー・シー・シャーウッド
タシル・シャムスル・ハーク
ショシャナ・エル・ポージー
スリーカンタ・ラトナ・クマール
ラクスマン・パスヌーリ
スブラマニア・ヘグデ
ルシト・クマール・アヌムラ
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Bristol Myers Squibb Co
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Bristol Myers Squibb Co
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4995—Pyrazines or piperazines forming part of bridged ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/12—Radicals substituted by oxygen atoms
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    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
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    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems
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    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08—Bridged systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Rheumatology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Indole Compounds (AREA)
JP2020534509A 2017-12-19 2018-12-18 Ｔｌｒ阻害剤として有用なアミド置換されたインドール化合物 Active JP7313354B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762607388P 2017-12-19 2017-12-19
US62/607,388 2017-12-19
PCT/US2018/066106 WO2019126081A1 (fr) 2017-12-19 2018-12-18 Composés d'indole à substitution amide utiles en tant qu'inhibiteurs de tlr

Publications (3)

Publication Number Publication Date
JP2021506923A JP2021506923A (ja) 2021-02-22
JP2021506923A5 JP2021506923A5 (fr) 2022-01-11
JP7313354B2 true JP7313354B2 (ja) 2023-07-24

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JP2020534509A Active JP7313354B2 (ja) 2017-12-19 2018-12-18 Ｔｌｒ阻害剤として有用なアミド置換されたインドール化合物

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Country Link
US (1) US11420973B2 (fr)
EP (1) EP3728221B1 (fr)
JP (1) JP7313354B2 (fr)
KR (1) KR20200101398A (fr)
CN (1) CN111511730B (fr)
AU (1) AU2018392316B2 (fr)
BR (1) BR112020011979A2 (fr)
CA (1) CA3085346A1 (fr)
EA (1) EA202091483A1 (fr)
ES (1) ES2922174T3 (fr)
IL (1) IL275353A (fr)
MX (1) MX2020005515A (fr)
SG (1) SG11202005700SA (fr)
WO (1) WO2019126081A1 (fr)

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US10071079B2 (en) 2016-06-29 2018-09-11 Bristol-Myers Squibb Company [1,2,4]triazolo[1,5-a]pyridinyl substituted indole compounds
EP3684767B1 (fr) 2017-09-22 2024-04-24 Jubilant Epipad LLC Composés hétérocycliques en tant qu'inhibiteurs de pad
FI3697785T3 (fi) 2017-10-18 2023-04-03 Jubilant Epipad LLC Imidatsopyridiiniyhdisteitä pad:n estäjinä
CN111386265A (zh) 2017-11-06 2020-07-07 朱比连特普罗德尔有限责任公司 作为pd1/pd-l1活化的抑制剂的嘧啶衍生物
IL274762B2 (en) 2017-11-24 2023-10-01 Jubilant Episcribe Llc Novel heterocyclic compounds as PRMT5 inhibitors
ES2904676T3 (es) * 2017-12-20 2022-04-05 Bristol Myers Squibb Co Compuestos de amino indol útiles como inhibidores de TLR
MX2020005622A (es) * 2017-12-20 2020-08-20 Bristol Myers Squibb Co Compuestos de indol sustituidos con arilo y heteroarilo.
KR20200131845A (ko) 2018-03-13 2020-11-24 주빌런트 프로델 엘엘씨 Pd1/pd-l1 상호작용/활성화 억제제로서의 비사이클릭 화합물
EP3807270B1 (fr) 2018-06-12 2023-09-13 F. Hoffmann-La Roche AG Nouveaux composés hétéroaryles hétérocyclyles pour le traitement d'une maladie auto-immune
EP3826724B1 (fr) 2018-07-23 2022-10-05 F. Hoffmann-La Roche AG Nouveaux composés de pipérazine pour le traitement d'une maladie auto-immune
EP3847169A1 (fr) 2018-09-04 2021-07-14 F. Hoffmann-La Roche AG Composés de benzothiazole pour le traitement de maladies auto-immunes
EP3847170B1 (fr) 2018-09-06 2022-06-22 F. Hoffmann-La Roche AG Nouveaux composés amidine cyclique pour le traitement d'une maladie auto-immune
WO2021087181A1 (fr) * 2019-11-01 2021-05-06 Bristol-Myers Squibb Company Composés de pyrazole substitués utilisés en tant qu'inhibiteurs du récepteur toll
AU2021214148A1 (en) * 2020-01-30 2022-07-14 Anima Biotech Inc. Collagen 1 translation inhibitors and methods of use thereof
US20230279001A1 (en) * 2020-08-04 2023-09-07 Hoffmann-La Roche Inc. Imidazo[1,2-a]pyridine compounds for the treatment of autoimmune disease
CR20230478A (es) 2021-04-16 2023-11-30 Gilead Sciences Inc Compuestos de tienopirrol.
CN114591339B (zh) * 2022-05-10 2022-08-02 上海维申医药有限公司 一类Toll样受体抑制剂及其制备和应用
KR20240066957A (ko) 2022-10-31 2024-05-16 아주대학교산학협력단 자기염증질환 치료 및 예방 조성물

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JP2003519101A (ja) 1999-10-26 2003-06-17 アベンティス・ファーマ・ドイチユラント・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング ＮＦκＢ活性を調節するための置換インドール
JP2005524621A (ja) 2002-01-07 2005-08-18 エーザイ株式会社 デアザプリンおよびそれらの用途
JP2006524668A (ja) 2003-04-25 2006-11-02 アヴェンティス ファーマ エス．エー． 新規なインドール誘導体、ならびに医薬物質および医薬組成物、特にｋｄｒ阻害剤としてのそれらの製造法
WO2010061903A1 (fr) 2008-11-27 2010-06-03 塩野義製薬株式会社 Dérivé de pyrimidine et dérivé de pyridine présentant tous deux une activité inhibitrice de pi3k
US20100249127A1 (en) 2009-03-31 2010-09-30 Arqule, Inc. Substituted indolo-pyridinone compounds
JP2011527692A (ja) 2008-07-08 2011-11-04 インテリカイン， インコーポレイテッド キナーゼインヒビターおよび使用方法
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